Preferred Language
Articles
/
7xc3kpIBVTCNdQwCSrdB
Preparation, <i>In-vitro, Ex-vivo</i>, and Pharmacokinetic Study of Lasmiditan as Intranasal Nanoemulsion-based <i>In Situ</i> Gel
...Show More Authors
Background:

Lasmiditan (LAS) is a recently developed antimigraine drug and was approved in October, 2019 for the treatment of acute migraines; however, it suffers from low oral bioavailability, which is around 40%.

Objective:

This study aimed to improve the LAS bioavailability via formulation as nanoemulsionbased in situ gel (NEIG) given intranasally and then compare the traditional aqueous-LASsuspension (AQS) with the two successful intranasal prepared formulations (NEIG 2 and NEIG 5) in order to determine its relative bioavailability (F-relative) via using rabbits.

Method:

Two successfully prepared nanoemulsion (NE) formulas, a and b, were selected for the incorporation of different percentages of pH-sensitive in situ gelling polymer (Carbopol 934) to prepare NEIGs 1, 2, 3, 4, 5, and 6. The pH, gelation capacity, gel strength, and viscosity were predicted for the prepared NEIGs. The release (in vitro) and the nasal permeation (ex vivo) were determined for NEIG 2 and 5, and then both were subjected to pharmacokinetics in vivo studies. Eighteen male rabbits weighing 2.0 to 2.5 kg were employed in the parallel design study. The body surface area (BSA) normalization method was applied for LAS dose calculation. Serial blood samples were taken out and subjected to drug analysis using the HPLC method previously developed and validated by Kumar et al. Primary pharmacokinetics parameters, including maximum drug concentration in plasma (Cmax), time to reach C-max (T-max), and area under the concentration-time curve from time zero to affinity (AUCt0-∞) were calculated. Both NE (a and b), together with NEIG (2 and 5) formulas, were subjected to the stability study. Finally, a nasal ciliotoxicity study was carried out to evaluate the nasal toxicity of developed NEIGs 2 and 5.

Result:

The results showed that NEIGs 2 and 5 could be selected as the optimized NEIGs as both achieved 100% permeation within 20 min and then released within 25 and 35 min, respectively, thus achieving 3.3 folds with higher permeation percentages as compared to the AQS. Both NEIGs 2 and 5 exerted comparable release and permeation values as the corresponding NE a and b with more residence time in order to overcome the normal nasal physiological clearance. The values of C-max, Tmax, and AUC0- ∞ for NEIG 2 and NEIG 5 were 8066 ± 242 ng/ml, 0.75 ± 0.05 h, 19616.86 ± 589 ng. h/ml, and 7975.67 ± 239 ng/ml, 1.0 ± 0.05 h, 17912.36 ± 537 ng. h/ml, respectively, compared to the traditional AQS, which is equal to 4181.09 ± 125 ng/ml, 2 ± 0.2 h, and 8852.27 ± 266 ng. h/ml, respectively. It was discovered that NEIGs 2 and 5 had better intranasal delivery of LAS and could significantly (p < 0.05) achieve a higher value of permeability coefficient (3.3 folds) and 2.5 folds improvement in bioavailability when compared to AQS. The NE a, NE b, NEIG2, and NEIG5 formulations showed good stability at various temperatures. According to the nasal ciliotoxicity study, the nasal mucosal membrane, which was treated with NEIG 5, showed irritation with a bit of damage. However, damage was not observed when it was treated with NEIG 2, indicating the biocompatibility of the last one to be selected as the optimum formula.

Conclusion:

NEIG 2 and NEIG 5 are promising new intranasal formulas with a faster onset of action and greater bioavailability than the oral dosage form (AQS). Finally, the selected optimum gold formula that will be ready for further clinical study is NEIG 2.

Scopus Crossref
View Publication
Publication Date
Sat Oct 12 2019
Journal Name
Iop Conf. Series: Journal Of Physics: Conf. Series
Preparation of Some (Transition Metal-Flavylium Salt- Flavon) Complexes
...Show More Authors

Three ligands were prepared, spectroscopic method and elemental analysis verified their structures. The L1 and L2 ligands are flavylium salts while the third one L3 is a Flavon. The reactions between transition metal salts and the ligands have synthesized two groups of new metal complexes, one group contains L1, L3 coordinated with the metal ion. The other group contains L2, L3 and the metal. These complexes have been identified by available spectroscopic tools (UV-Visible and IR), the C.H.N results confirmed the proposed structures. The experimental data disclosed that the complexes were coordinated by 6the coordinate with mono-and bidentate ligands forming octahedral structure, in which L3 acts as monodentate and L1, L2 as bidentate ligan

... Show More
Preview PDF
Publication Date
Sat Jun 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Preparation of Posaconazole Nanosponges for Improved Topical Delivery System
...Show More Authors

The objective of the current research was to develop the posaconazole (PCZ) loaded NS into the carbopol 934 polymeric gel for prolonged drug release and improved topical delivery; seven different nanosponge formulations of PCZ were formulated using the emulsion solvent diffusion method using various amounts of polymer (ethylcellulose, EC). The aqueous and dispersed phases were prepared using polyvinyl alcohol (PVA) and dichloromethane. The prepared nanosponges (NS) were studied for particle size, structural appearance, and in vitro drug release. Furthermore, the selected formula was formulated as hydrogel and was evaluated for physical characteristics, drug content, and in-vitro drug release. Morphological studies revealed irregular

... Show More
View Publication
Scopus (9)
Crossref (7)
Scopus Crossref
Publication Date
Thu Dec 01 2022
Journal Name
Iraqi Journal Of Physics
Preparation of Silicon Nanowires Photocathode for Photoelectrochemical Water Splitting
...Show More Authors

A metal-assisted chemical etching process employing p-type silicon wafers with varied etching durations is used to produce silicon nanowires. Silver nanoparticles prepared by chemical deposition are utilized as a catalyst in the formation of silicon nanowires. Images from field emission scanning electron microscopy confirmed that the diameter of SiNWs grows when the etching duration is increased. The photoelectrochemical cell's characteristics were investigated using p-type silicon nanowires as working electrodes. Linear sweep voltammetry (J-V) measurements on p-SiNWs confirmed that photocurrent density rose from 0.20 mA cm-2 to 0.92 mA cm-2 as the etching duration of prepared SiNWs increased from 15 to 30 min. The

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Sep 08 2020
Journal Name
Baghdad Science Journal
Optimization of nanostructured/nano sized rice husk ash preparation
...Show More Authors

The objective of the study is developing a procedure for production and characterization of rice husk ash (RHA). The effects of rice husk (RH) amount, burning/cooling conditions combined with stirring on producing of RHA with amorphous silica, highest SiO2, lowest loss on ignition (LOI), uniform particle shape distribution and nano structured size have been studied. It is concluded that the best amount is 20 g RH in 125 ml evaporating dish Porcelain with burning for 2 h at temperature 700 °C combined with cooling three times during burning to produce RHA with amorphous silica, SiO2 90.78% and LOI 1.73%. On the other hand, cooling and stirring times affect the variation of nano structured size and particle shape dis

... Show More
View Publication Preview PDF
Scopus (2)
Crossref (2)
Scopus Clarivate Crossref
Publication Date
Tue Dec 30 2014
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
PREPARATION OF PVC HOLLOW FIBER MEMBRANE USING (DMAC/ACETONE)
...Show More Authors

Membrane manufacturing system was operated using dry/wet phase inversion process. A sample of hollow fiber membrane was prepared using (17% wt PVC) polyvinyl chloride as membrane material and N, N Dimethylacetamide (DMAC) as solvent in the first run and the second run was made using (DMAC/Acetone) of ratio 3.4 w/w. Scanning electron microscope (SEM) was used to predict the structure and dimensions of hollow fiber membranes prepared. The ultrafiltration experiments were performed using soluble polymeric solute poly ethylene glycol (PEG) of molecular weight (20000 Dalton) 800 ppm solution 25 °C temperature and 1 bar pressure. The experimental results show that pure water permeation increased from 25.7 to 32.2 (L/m2.h.bar) by adding a

... Show More
View Publication
Crossref
Publication Date
Wed Dec 30 2009
Journal Name
Iraqi Journal Of Physics
Preparation of Polyvinyl Alcohol/ Tio2 Nano Fiber by Electrospinning
...Show More Authors

In this research we prepared nanofibers by electrospinning from
poly (Vinyl Alcohol) /TiO2. The spectrum of the solution (Emission)
was studied and found to be at 772 nm, several process parameters
were such as concentration of TiO2 , and the effect of distance from
nozzle tip to the grounded collector (gap distance). The result of the
lower concentration of, the smaller the diameter of nanofiber is.
Increasing the gap distance will affect nanofibers diameter

View Publication Preview PDF
Publication Date
Mon Jun 01 2015
Journal Name
Journal Of Engineering
Laboratory Preparation of Simulated Sludge for Anaerobic Digestion Experimentation
...Show More Authors

Health and environmental factors as well as operational difficulties are major challenges facing the development of an anaerobic digestion process. Some of these problems relate to the use of sludge collected from primary and secondary clarifier units in wastewater treatment plants for laboratory purposes.

The present study addresses the preparation of sludge for laboratory purposes by using a mixture that consists of the digested sludge, which is less pathogenic, compared to the collected sludge from the primary or secondary clarifier, and food wastes. The sludge has been tested experimentally for 19 and 32 days under mesophilic conditions. The results show a steady methane production rate from the anaerobic dig

... Show More
View Publication Preview PDF
Publication Date
Tue Dec 30 2014
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
PREPARATION OF PVC HOLLOW FIBER MEMBRANE USING (DMAC/ACETONE)
...Show More Authors

Membrane manufacturing system was operated using dry/wet phase inversion process. A sample of hollow fiber membrane was prepared using (17% wt PVC) polyvinyl chloride as membrane material and N, N Dimethylacetamide (DMAC) as solvent in the first run and the second run was made using (DMAC/Acetone) of ratio 3.4 w/w. Scanning electron microscope (SEM) was used to predict the structure and dimensions of hollow fiber membranes prepared. The ultrafiltration experiments were performed using soluble polymeric solute poly ethylene glycol (PEG) of molecular weight (20000 Dalton) 800 ppm solution 25 °C temperature and 1 bar pressure. The experimental results show that pure water permeation increased from 25.7 to 32.2 (L/m2.h.bar) by adding aceton

... Show More
View Publication Preview PDF
Publication Date
Tue Sep 01 2009
Journal Name
Iraqi Journal Of Physics
Preparation of Polyvinyl Alcohol/ Tio2 Nano Fiber by Electrospinning
...Show More Authors

ِabstract:In this research we prepared nanofibers by electrospinning from poly (Vinyl Alcohol) /TiO2. The spectrum of the solution (Emission) was studied and found to be at 772 nm, several process parameters were such as concentration of TiO2 , and the effect of distance from nozzle tip to the grounded collector (gap distance). The result of the lower concentration of, the smaller the diameter of nanofiber is. Increasing the gap distance will affect nanofibers diameter.

Preview PDF
Publication Date
Fri Feb 23 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Phytochemical and Pharmacological Study of Valepotriates in Valeriana officinalis L. F.Valerianeceae Cultivated in Iraq
...Show More Authors

This study concerned with phytochemical investigation and methods of extraction and separation of active constituents from Valeriana officinalis plant cultivated in Iraq. Due to the large number of active constituents in Valeriana officinalis, it was necessary to make analytical study of its constituents to determine the chemical nature of these constituents and then determine the main classes (terpenes and iridoids) using chemical reagents specific for each class. Different organic solvents like ethanol (70%) used in soxhlet apparatus and hexane, ethyl acetate and methanol were used separately to extract the main active constituents by maceration. Through comparison between these solvents using thin layer chromatograph

... Show More
View Publication Preview PDF
Crossref (1)
Crossref